193275-84-2
Chemical Structure
Lonafarnib
Synonym(s): Sch66336
- CAS No.: 193275-84-2
- Formula:C27H31Br2ClN4O2
- Molecular Weight:638.82
IUPAC Name: (R)-4-(2-(4-(3,10-dibromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperidin-1-yl)-2-oxoethyl)piperidine-1-carboxamide
InChIKey: DHMTURDWPRKSOA-RUZDIDTESA-N
SMILES: O=C(N)N1CCC(CC1)CC(N2CCC(CC2)[C@@H]3C4=C(C=C(C=C4CCC5=CC(Br)=CN=C53)Cl)Br)=O
Biological Activity: Lonafarnib (Sch66336) is a potent and orally active, and CNS-penetrant farnesyl transferase (FTase) inhibitor. Lonafarnib inhibits the activities of H-ras, K-ras and N-ras with IC50 values of 1.9 nM, 5.2 nM and 2.8 nM, respectively. Lonafarnib also has anti-hepatitis delta virus (HDV) activities[1][2][3][4].
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Lonafarnib | 99.85% | Lonafarnib (Sch66336) is a potent and orally active, and CNS-penetrant farnesyl transferase (FTase) inhibitor. Lonafarnib inhibits the activities of H-ras, K-ras and N-ras with IC50 values of 1.9 nM, 5.2 nM and 2.8 nM, respectively. Lonafarnib also has anti-hepatitis delta virus (HDV) activities. | ||||||||||||||||||||
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Lonafarnib (Standard) | ≥98% | Lonafarnib (Standard) is the analytical standard of Lonafarnib. This product is intended for research and analytical applications. Lonafarnib (Sch66336) is a potent and orally active farnesyl transferase (FTase) inhibitor. Lonafarnib inhibits the activities of H-ras, K-ras and N-ras with IC50 values of 1.9 nM, 5.2 nM and 2.8 nM, respectively. Lonafarnib also has anti-hepatitis delta virus (HDV) activities. | ||||||||||||||||||||
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- [1]. Liu M, et al. Antitumor activity of SCH 66336, an orally bioavailable tricyclic inhibitor of farnesyl protein transferase, in human tumor xenograft models and wap-ras transgenic mice. Cancer Res. 1998 Nov 1;58(21):4947-56. [Content Brief]
- [2]. Chaponis D, et al. Lonafarnib (SCH66336) improves the activity of temozolomide and radiation for orthotopic malignant gliomas. J Neurooncol. 2011 Aug;104(1):179-89. [Content Brief]
- [3]. Koh C,et al. Oral prenylation inhibition with lonafarnib in chronic hepatitis D infection: a proof-of-concept randomised, double-blind, placebo-controlled phase 2A trial. Lancet Infect Dis. 2015 Oct;15(10):1167-1174. [Content Brief]
- [4]. Hernandez I, et al. A farnesyltransferase inhibitor activates lysosomes and reduces tau pathology in mice with tauopathy. Sci Transl Med. 2019 Mar 27;11(485):eaat3005. [Content Brief]
Keywords
